We have previously demonstrated the ability of the 2-azabicyclo-(2.2.2)octane ring system to serve as a rigid nucleus for receptor topography studies. Additionally, our earlier hypothesis that this ring system would also serve to impart enhanced biological activity to the analogs studied over rigid analogs previously reported was confirmed. The interesting and unique biological activity found for our analogs of acetylcholine, procaine, and the prodine analgetics prompts us to seek support for an expansion of our earlier studies. We are proposing here the synthesis of analogs of basic anilide analgetics, analgetic antagonists, antihistaminics, CNS stimulants, and CNS depressants, the pharmacological evaluation of these analogs, and the resolution of biologically active racemic mixtures. We suggest that the proposed analogs could possess useful pharmacological profiles while at the same time provide valuable information regarding the nature of receptor binding of prototype drugs. BIBLIOGRAPHIC REFERENCES: J. C. Murphy, E. S. Watson, P. W. Wirth, C. R. Clark and R. F. Borne, "Conformational Aspects of the Antifibrillatory Activity of Procaine, Eur. J. Pharmacol., 40, 359 (1976). R. F. Borne, J. A. Bedford, J. L. Buelke, C. B. Craig, T. C. Hardin, A. H. Kibbe and M. C. Wilson, "Biological Effects of Cocaine Derivatives I: Improved Synthesis and Pharmacological Evaluation of Norcocaine," J. Pharm. Sci., 66, 119 (1977).